DERIVATIVES OF IMIDAZOLE, PHARMACEUTICAL COMPOSITION, AND METHODS FOR INHIBITION OF ACTIVITY OF FARNESYL PROTEIN TRANSFERASE AND PRENYLTRANS- FERASE AND SUPPRESSION OF TUMOR GROWTH Russian patent published in 2003 - IPC

Abstract RU 2211838 C2

FIELD: organic chemistry, biochemistry, medicine, oncology. SUBSTANCE: invention relates to novel derivatives of imidazole of the formulas (I) and (II) wherein l, m, r, s and t = 0 or 1; n = 1 or 2 under condition that when l and m = 0 then n = 2; Y means SO2 or CH2; Z means CR12,NR32SO2,NR13,NR36CO,OCONR15,SO2NR14; R1 is taken among the group consisting of hydrogen atom, alkyl or aralkyl and symbol means a simple or double bond; R7,R8 are taken among the group consisting of hydrogen atom, aryl, -CN, halide and U-R44 where U means oxygen atom; R44 and R11 are taken among the group consisting of hydrogen atom, alkyl, aralkyl, aryl; R32 is taken among the group consisting of hydrogen atom, unsubstituted lower alkyl or lower alkyl substituted with phenyl and thienyl; R9,R10,R12,R13,R14,R15,R36,R37,R38 represent hydrogen atom or lower alkyl; one of R, S and T represents CH2 or CH(CH2)pQ where Q means NR57R58 wherein p = 0, 1 or 2 under condition that when Y means SO2 then R11 can not mean hydrogen atom. Invention relates also to its enantiomers, diastereomers, pharmaceutically acceptable salts and solvates. Invention relates also to pharmaceutical composition based on these compounds, methods for inhibition of activity of farnesyl protein transferase and prenyltranseferase and inhibition of the tumor growth. Invention provides preparing novel derivatives of imidazole eliciting inhibitory activity with respect to farnesyl protein transferase and prenyl- transferase and usable for suppression of growth of tumors. EFFECT: improved inhibition methods, valuable medicinal properties of compounds. 14 cl, 1 tbl, 30 ex

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RU 2 211 838 C2

Authors

Bkhajd Radzhiv S.

Ding Charlz Z.

Khant Dzhon T.

Kim Sung-Khun

Lefteris Katrina

Dates

2003-09-10Published

1998-06-16Filed